药物动力学trapidil,血小板衍生生长因子的拮抗剂,在健康受试者和肝硬化患者。
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困难年代,Thurmann PA,泛滥,Benjaminov
药物动力学trapidil,血小板衍生生长因子的拮抗剂,在健康受试者和肝硬化患者。
Br中国新药杂志。1996年10月,42 (4):443 - 9。
- PubMed ID
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8904615 (在PubMed]
- 文摘
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1。trapidil的药代动力学参数(血小板衍生生长因子的拮抗剂)进行评估12个健康男性受试者(研究)和一组10肝硬化患者(儿童B)和五个对照组,分别(研究二)。2。调查后进行单剂量trapidil(200毫克)和稳态后应用200毫克trapidil连续5天每天三次(研究1)或4天(研究二)。3。研究我:终端消除trapidil阶段的浓度时间曲线表现出轻微的凸性这可能反映非线性动力学。后的AUC trapidil获得第一剂量(20.5(+ / - 7.0南达科他州。]micrograms ml-1 h) was markedly higher than the AUC determined at steady state (13.2 [+/- 3.8 s.d.] micrograms ml-1 h), the non-parametric 90% confidence intervals of the ratio day 5/day 1 was 0.58-0.73 (point estimator 0.64). 4. Study II: AUC averaged (21.4 [+/- 9.1 s.d.] micrograms ml-1 h) in controls and (34.4 [+/- 14.9 s.d.] micrograms ml-1 h) in cirrhotic patients. The 90% confidence intervals for the difference group 1 vs group 2 was 0.95-2.97 (point estimator 1.48, P = 0.066). At steady state, AUC averaged (13.7 [+/- 5.7 s.d.] micrograms ml-1 h) in controls and (20.8 [+/- 6.8 s.d.] micrograms ml-1 h) in cirrhotic patients (90% confidence intervals group 1 vs group 2: 0.88-2.20 [point estimator 1.45, P = 0.05]). As seen in study I, the AUC of trapidil obtained after the first dose was markedly higher than the AUC determined at steady state, the non-parametric 90% confidence intervals of the ratio day 5/day 1 was 0.48-0.84 (point estimator 0.66) in control subjects and 0.54-0.72 (point estimator 0.64) in cirrhotic patients, respectively. 5. An inverse correlation was seen between the results of the monoethylglycinxilidid (MEGX)-test and the AUC of trapidil (single dose: r = -0.516, P = 0.048; steady state: r = -0.548, P = 0.042). 6. Results of study I and study II indicate an autoinduction of trapidil metabolism after repeated oral doses. Although trapidil elimination is decreased in patients with liver cirrhosis (study II), the elimination half-life at steady state is relatively short (2.4 [+/- 1.1 s.d.] h) and therefore should prevent cumulation of trapidil even in cirrhotic patients.
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